Rhosin (hydrochloride)

Rho-GEF蛋白质-蛋白质相互作用的抑制剂；在10和30µM时抑制RhoA活性；选择性地减少MCF-7乳腺癌细胞乳球的数量和大小，而减少MCF-10A非癌细胞乳球的数量和大小；抑制表达RhoC的MCF-7细胞和人类乳腺上皮细胞的迁移和侵袭；在30µM时增加PC12细胞中的神经突生长；在抑郁小鼠模型中，以40mg/kg的剂量施用，可防止社交失败压力引起的过度兴奋，并增加D1-MSN中的脊柱密度；在抑郁小鼠模型中，可防止社交失败压力引起的社交回避，并减少蔗糖偏好。An inhibitor of the Rho-GEF protein-protein interaction; inhibits RhoA activity at 10 and 30 µM; selectively reduces the number and size of MCF-7 breast cancer cell mammospheres over MCF-10A non-cancerous cell mammospheres; inhibits migration and invasion of MCF-7 cells and human mammary epithelial cells expressing RhoC; increases neurite outgrowth in PC12 cells at 30 µM; prevents social defeat stress-induced hyperexcitability and increases spine density in D1-MSNs when administered post-social defeat stress in a mouse model of depression at 40 mg/kg; prevents social defeat stress-induced social avoidance and reductions in sucrose preference in a mouse model of depression.分子式C20H18N6O • HCl分子量394.9O=C(N/N=C/C1=CC2=C(N=CC=N2)C=C1)[C@H](N)CC3=CNC4=CC=CC=C34.Cl